In 2020.0 BIOORG CHEM published article about CELL-GROWTH INHIBITORS; CYCLOOXYGENASE-2 INHIBITORS; BIOLOGICAL EVALUATION; ALPHA; CONSEQUENCES; METABOLISM; ANALOGS in [Abdel-Halim, Mohammad; Weam, Mohammed; Atta, Noha H.; Hammam, Mennatallah A.; Hefnawy, Amr; Abadi, Ashraf H.] German Univ Cairo, Fac Pharm & Biotechnol, Dept Pharmaceut Chem, Cairo 11835, Egypt; [Tinsley, Heather] Univ Montevallo, Dept Biol, Montevallo, AL USA; [Keeton, Adam B.; Piazza, Gary A.] Univ S Alabama, Mitchell Canc Inst, Dept Pharmacol, Drug Discovery Res Ctr, Mobile, AL 36608 USA; [Hartmann, Rolf W.; Engel, Matthias] Saarland Univ, Pharmaceut & Med Chem, Campus C2-3, D-66123 Saarbrucken, Germany in 2020.0, Cited 44.0. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7. HPLC of Formula: C9H10O3
Celecoxib, is a selective cyclooxygenase-2 (COX2) inhibitor with a 1,5-diaryl pyrazole scaffold. Celecoxib has a better safety profile compared to other COX2 inhibitors having side effects of systemic hypertension and thromboembolic complications. This may be partly attributed to an off-target activity involving phosphodiesterase 5 (PDE5) inhibition and the potentiation of NO/cGMP signalling allowing coronary vasodilation and aortic relaxation. Inspired by the structure of celecoxib, we synthesized a chemically diverse series of compounds containing a 1,3,5-trisubstituted pyrazoline scaffold to improve PDE5 inhibitory potency, while eliminating COX2 inhibitory activity. SAR studies for PDE5 inhibition revealed an essential role for a carboxylic acid functionality at the 1-phenyl and the importance of the non-planar pyrazoline core over the planar pyrazole with the 5-phenyl moiety tolerating a range of substituents. These modifications led to new PDE5 inhibitors with approximately 20-fold improved potency to inhibit PDE5 and no COX-2 inhibitory activity compared with celecoxib. PDE isozyme profiling of compound 11 revealed a favorable selectivity profile. These results suggest that trisubstituted pyrazolines provide a promising scaffold for further chemical optimization to identify novel PDE5 inhibitors with potential for less side effects compared with available PDE5 inhibitors used for the treatment of penile erectile dysfunction and pulmonary hypertension.
Welcome to talk about 93-02-7, If you have any questions, you can contact Abdel-Halim, M; Tinsley, H; Keeton, AB; Weam, M; Atta, NH; Hammam, MA; Hefnawy, A; Hartmann, RW; Engel, M; Piazza, GA; Abadi, AH or send Email.. HPLC of Formula: C9H10O3
Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com